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Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. doi: 10.1016/j.bmcl.2010.04.071. Epub 2010 Apr 21.

Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

Abstract

Synthesis and structure-activity relationships of cannabinoid-1 receptor (CB1R) inverse agonists based on dihydro-pyrano[2,3-b] pyridine and tetrahydro-1,8-naphtyridine scaffolds are presented. Rat food intake and pharmacokinetic evaluation of 13g, 13i, 13k and 17a revealed these compounds to be highly efficacious orally active modulators of CB1R.

PMID:
20483606
DOI:
10.1016/j.bmcl.2010.04.071
[Indexed for MEDLINE]

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